The interaction of nivazol with the glucocorticoid receptor from rat and rhesus monkey target tissues
Steroid hormone receptor competition techniques were used to evaluate the glucocorticoid receptor binding properties of nivazol and its 11β-hydroxy derivative, Win 44577 in rat and monkey target tissues. These agents competitively inhibited the binding of 3H-dexamethasone to the glucocorticoid recep...
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| Veröffentlicht in: | Steroids 1984-11, Vol.44 (5), p.447-457 |
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| container_end_page | 457 |
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| container_issue | 5 |
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| container_title | Steroids |
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| creator | Winneker, Richard C. Russell, Margaret M. Might, Christine K. Schane, H. Philip |
| description | Steroid hormone receptor competition techniques were used to evaluate the glucocorticoid receptor binding properties of nivazol and its 11β-hydroxy derivative, Win 44577 in rat and monkey target tissues. These agents competitively inhibited the binding of
3H-dexamethasone to the glucocorticoid receptor from the liver and anterior pituitary from both rat and monkey with relative binding affinities of Win 44577 > dexamethasone >nivazol >cortisol in all cases. However, nivazol and Win 44577 had approximately twice the affinity for the anterior pituitary glucocorticoid receptor from both species. Neither compound demonstrated any significant binding to rat estrogen, progestin or androgen receptors. These results are consistent with a glucocorticoid receptor mediated mechanism of action for nivazol and Win 44577; however, the difference in the endocrine profile of nivazol in the rhesus monkey versus the rat does not appear to be due to a species selectivity in the affinity of nivazol for the glucocorticoid receptor from central or peripheral target tissue. |
| doi_str_mv | 10.1016/S0039-128X(84)80004-5 |
| format | Article |
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3H-dexamethasone to the glucocorticoid receptor from the liver and anterior pituitary from both rat and monkey with relative binding affinities of Win 44577 > dexamethasone >nivazol >cortisol in all cases. However, nivazol and Win 44577 had approximately twice the affinity for the anterior pituitary glucocorticoid receptor from both species. Neither compound demonstrated any significant binding to rat estrogen, progestin or androgen receptors. These results are consistent with a glucocorticoid receptor mediated mechanism of action for nivazol and Win 44577; however, the difference in the endocrine profile of nivazol in the rhesus monkey versus the rat does not appear to be due to a species selectivity in the affinity of nivazol for the glucocorticoid receptor from central or peripheral target tissue.</description><identifier>ISSN: 0039-128X</identifier><identifier>EISSN: 1878-5867</identifier><identifier>DOI: 10.1016/S0039-128X(84)80004-5</identifier><identifier>PMID: 6549568</identifier><identifier>CODEN: STEDAM</identifier><language>eng</language><publisher>New York, NY: Elsevier Inc</publisher><subject>Animals ; Binding, Competitive ; Biological and medical sciences ; Dexamethasone - metabolism ; Female ; Hormones. Endocrine system ; Hydrocortisone - metabolism ; In Vitro Techniques ; Liver - metabolism ; Macaca mulatta ; Male ; Medical sciences ; Pharmacology. Drug treatments ; Pituitary Gland, Anterior - metabolism ; Pregnadienediols - metabolism ; Pregnadienes - metabolism ; Rats ; Receptors, Glucocorticoid - metabolism ; Species Specificity</subject><ispartof>Steroids, 1984-11, Vol.44 (5), p.447-457</ispartof><rights>1984</rights><rights>1986 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c389t-2b8f412713a4d48bc9bbfe80940b9747dc771e23a136007696070da753065b0d3</citedby><cites>FETCH-LOGICAL-c389t-2b8f412713a4d48bc9bbfe80940b9747dc771e23a136007696070da753065b0d3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://www.sciencedirect.com/science/article/pii/S0039128X84800045$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,776,780,3536,27903,27904,65309</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=8578080$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/6549568$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Winneker, Richard C.</creatorcontrib><creatorcontrib>Russell, Margaret M.</creatorcontrib><creatorcontrib>Might, Christine K.</creatorcontrib><creatorcontrib>Schane, H. Philip</creatorcontrib><title>The interaction of nivazol with the glucocorticoid receptor from rat and rhesus monkey target tissues</title><title>Steroids</title><addtitle>Steroids</addtitle><description>Steroid hormone receptor competition techniques were used to evaluate the glucocorticoid receptor binding properties of nivazol and its 11β-hydroxy derivative, Win 44577 in rat and monkey target tissues. These agents competitively inhibited the binding of
3H-dexamethasone to the glucocorticoid receptor from the liver and anterior pituitary from both rat and monkey with relative binding affinities of Win 44577 > dexamethasone >nivazol >cortisol in all cases. However, nivazol and Win 44577 had approximately twice the affinity for the anterior pituitary glucocorticoid receptor from both species. Neither compound demonstrated any significant binding to rat estrogen, progestin or androgen receptors. These results are consistent with a glucocorticoid receptor mediated mechanism of action for nivazol and Win 44577; however, the difference in the endocrine profile of nivazol in the rhesus monkey versus the rat does not appear to be due to a species selectivity in the affinity of nivazol for the glucocorticoid receptor from central or peripheral target tissue.</description><subject>Animals</subject><subject>Binding, Competitive</subject><subject>Biological and medical sciences</subject><subject>Dexamethasone - metabolism</subject><subject>Female</subject><subject>Hormones. Endocrine system</subject><subject>Hydrocortisone - metabolism</subject><subject>In Vitro Techniques</subject><subject>Liver - metabolism</subject><subject>Macaca mulatta</subject><subject>Male</subject><subject>Medical sciences</subject><subject>Pharmacology. Drug treatments</subject><subject>Pituitary Gland, Anterior - metabolism</subject><subject>Pregnadienediols - metabolism</subject><subject>Pregnadienes - metabolism</subject><subject>Rats</subject><subject>Receptors, Glucocorticoid - metabolism</subject><subject>Species Specificity</subject><issn>0039-128X</issn><issn>1878-5867</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1984</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkE1rFTEUhoMo9bb6EwpZiOhi9GQmnyspRatQcGEFdyGTOdMbnZlck0yl_nrT3svdujpw3ud88BByzuAdAybffwPoTMNa_eON5m81APBGPCEbppVuhJbqKdkckefkNOeflZGdaU_IiRTcCKk3BG-2SMNSMDlfQlxoHOkS7tzfONE_oWxpqfnttProYyrBxzDQhB53JSY6pjjT5Ap1S-1uMa-ZznH5hfe0uHSLhZaQ84r5BXk2uinjy0M9I98_fby5_Nxcf736cnlx3fhOm9K0vR45axXrHB-47r3p-xE1GA69UVwNXimGbedYJwGUNBIUDE6JDqToYejOyOv93l2Kv-vdYueQPU6TWzCu2SphpOx4W0GxB32KOScc7S6F2aV7y8A-6LWPeu2DO6u5fdRrRZ07PxxY-xmH49TBZ81fHXKXvZvG5BYf8hHTQmnQULEPewyrjLuAyWYfcPE4hCq32CGG_zzyDzEll-k</recordid><startdate>198411</startdate><enddate>198411</enddate><creator>Winneker, Richard C.</creator><creator>Russell, Margaret M.</creator><creator>Might, Christine K.</creator><creator>Schane, H. 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Endocrine system</topic><topic>Hydrocortisone - metabolism</topic><topic>In Vitro Techniques</topic><topic>Liver - metabolism</topic><topic>Macaca mulatta</topic><topic>Male</topic><topic>Medical sciences</topic><topic>Pharmacology. Drug treatments</topic><topic>Pituitary Gland, Anterior - metabolism</topic><topic>Pregnadienediols - metabolism</topic><topic>Pregnadienes - metabolism</topic><topic>Rats</topic><topic>Receptors, Glucocorticoid - metabolism</topic><topic>Species Specificity</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Winneker, Richard C.</creatorcontrib><creatorcontrib>Russell, Margaret M.</creatorcontrib><creatorcontrib>Might, Christine K.</creatorcontrib><creatorcontrib>Schane, H. 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Philip</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>The interaction of nivazol with the glucocorticoid receptor from rat and rhesus monkey target tissues</atitle><jtitle>Steroids</jtitle><addtitle>Steroids</addtitle><date>1984-11</date><risdate>1984</risdate><volume>44</volume><issue>5</issue><spage>447</spage><epage>457</epage><pages>447-457</pages><issn>0039-128X</issn><eissn>1878-5867</eissn><coden>STEDAM</coden><abstract>Steroid hormone receptor competition techniques were used to evaluate the glucocorticoid receptor binding properties of nivazol and its 11β-hydroxy derivative, Win 44577 in rat and monkey target tissues. These agents competitively inhibited the binding of
3H-dexamethasone to the glucocorticoid receptor from the liver and anterior pituitary from both rat and monkey with relative binding affinities of Win 44577 > dexamethasone >nivazol >cortisol in all cases. However, nivazol and Win 44577 had approximately twice the affinity for the anterior pituitary glucocorticoid receptor from both species. Neither compound demonstrated any significant binding to rat estrogen, progestin or androgen receptors. These results are consistent with a glucocorticoid receptor mediated mechanism of action for nivazol and Win 44577; however, the difference in the endocrine profile of nivazol in the rhesus monkey versus the rat does not appear to be due to a species selectivity in the affinity of nivazol for the glucocorticoid receptor from central or peripheral target tissue.</abstract><cop>New York, NY</cop><pub>Elsevier Inc</pub><pmid>6549568</pmid><doi>10.1016/S0039-128X(84)80004-5</doi><tpages>11</tpages></addata></record> |
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| ispartof | Steroids, 1984-11, Vol.44 (5), p.447-457 |
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| source | MEDLINE; Elsevier ScienceDirect Journals |
| subjects | Animals Binding, Competitive Biological and medical sciences Dexamethasone - metabolism Female Hormones. Endocrine system Hydrocortisone - metabolism In Vitro Techniques Liver - metabolism Macaca mulatta Male Medical sciences Pharmacology. Drug treatments Pituitary Gland, Anterior - metabolism Pregnadienediols - metabolism Pregnadienes - metabolism Rats Receptors, Glucocorticoid - metabolism Species Specificity |
| title | The interaction of nivazol with the glucocorticoid receptor from rat and rhesus monkey target tissues |
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